Patent SG-11201909115W-A (SG)
Title: Tricyclic compounds as glycogen synthase kinase 3 (gsk3) inhibitors and uses thereof
Inventor: WAGNER FLORENCE
IPC: C07D471/10
Filed: 2018-04-05
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 1111111111110110101011111011010 I 0111 10111111111001101110111 10# (10) International Publication Number WO 2018/187630 A8 11 October 2018 (11.10.2018) WIPO I PCT (51) International Patent Classification: A61K 31/4745 (2006.01) CO7D 471/10 (2006.01) CO7D 471/04 (2006.01) (21) International Application Number: PCT/US2018/026339 (22) International Filing Date: 05 April 2018 (05.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/481,981 05 April 2017 (05.04.2017) US MA INC. [US/US]; 225 Binney Street, Cambridge, MA 02142 (US). (72) Inventors: WAGNER, Florence, Fevrier; 4 Old Coun- try Path, Ashland, MA 01721 (US). WEIWER, Michel; 18 Hunting Street, Apt 1, Cambridge, MA 02141 (US). CAMPBELL, Arthur, J; 189 Lexington Avenue, Cam- bridge, MA 02138 (US). SACHER, Joshua, R.; 40 Marion Street, Somerville, MA 02143 (US). HOLSON, Edward; 66 Forest Street, Newton, MA 02461 (US). LUCAS, Bri- an, Stuart; 4 Brantwood Road, Arlington, MA 02476 (US). CHEN, TeYu; 8 Brighton Street Unit 1, Charlestown, MA 02129 (US). Agent: ZHANG, Wei; Wolf, Greenfield & Sacks, P.C., 600 Atlantic Avenue, Boston, MA 02210-2206 (US). (74) (71) Applicants: THE BROAD INSTITUTE, INC. [US/US]; 415 Main Street, Cambridge, MA 02142 (US). BIOGEN (54) Title: TRICYCLIC COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 (GSK3) INHIBITORS AND USES THEREOF FIG.3 (1) GC O er) N GC 1-1 00 O 1-1 N O (57) : The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tau- tomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intel- lectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder). [Continued on next page] WO 2018/187630 A8 MIDEDIMOMOIDEIREEMOMOHOEHROMMEME# (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (48) Date of publication of this corrected version: 03 January 2019 (03.01.2019) (15) Information about Correction: see Notice of 03 January 2019 (03.01.2019)